Purine Synthesis Inhibitors (PSI)

FLAG’s Purine Synthesis Inhibitors (PSI) are novel compounds meticulously designed to avoid uptake by the ubiquitous RFC and to enter cells only via receptor sites that are over-expressed on cancer cells (e.g., folate receptor alpha, beta and PCFT), leaving normal cells intact.

purine synthesis inhibitor


PSI’s are designed to impart cytotoxicity via potent inhibition of β-glycinamide ribonucleotide formyltransferase (GARFTase), which catalyzes the first folate-dependent reaction in de novo purine nucleotide biosynthesis as well as inhibits one-carbon mitochondrial processing via SHMT-1 and SHMT-2 inhibition.